EP4076492A4 - Pcsk9 antagonist compounds - Google Patents
Pcsk9 antagonist compoundsInfo
- Publication number
- EP4076492A4 EP4076492A4 EP20901412.5A EP20901412A EP4076492A4 EP 4076492 A4 EP4076492 A4 EP 4076492A4 EP 20901412 A EP20901412 A EP 20901412A EP 4076492 A4 EP4076492 A4 EP 4076492A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- antagonist compounds
- pcsk9 antagonist
- pcsk9
- compounds
- antagonist
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 101150094724 PCSK9 gene Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
- C12N9/6424—Serine endopeptidases (3.4.21)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
- C12Y304/21—Serine endopeptidases (3.4.21)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- General Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962951802P | 2019-12-20 | 2019-12-20 | |
PCT/US2020/066046 WO2021127460A1 (en) | 2019-12-20 | 2020-12-18 | Pcsk9 antagonist compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
EP4076492A1 EP4076492A1 (en) | 2022-10-26 |
EP4076492A4 true EP4076492A4 (en) | 2024-01-17 |
Family
ID=76478335
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP20901412.5A Pending EP4076492A4 (en) | 2019-12-20 | 2020-12-18 | Pcsk9 antagonist compounds |
Country Status (3)
Country | Link |
---|---|
US (1) | US20230144324A1 (en) |
EP (1) | EP4076492A4 (en) |
WO (1) | WO2021127460A1 (en) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3810176A4 (en) | 2018-06-21 | 2022-05-18 | RA Pharmaceuticals, Inc. | Cyclic polypeptides for pcsk9 inhibition |
US11814445B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
WO2021041770A1 (en) * | 2019-08-30 | 2021-03-04 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist compounds |
US11932705B2 (en) | 2020-12-18 | 2024-03-19 | Merck Sharp & Dohme Llc | Cyclic polypeptides for PCSK9 inhibition |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013041678A1 (en) * | 2011-09-23 | 2013-03-28 | Novo Nordisk A/S | Novel glucagon analogues |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5104869A (en) * | 1989-10-11 | 1992-04-14 | American Cyanamid Company | Renin inhibitors |
US20110301079A1 (en) * | 2007-09-21 | 2011-12-08 | Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Neuromedin u receptor agonists and uses thereof |
BR112018076242A2 (en) * | 2016-06-24 | 2019-03-26 | Hoffmann La Roche | pcsk9 inhibitors, inhibited pcsk9, pharmaceutical composition, methods to modulate pcsk9 activity, to inhibit binding of pcsk9 to ldlr, to increase ldlr availability, to reduce ldl-c level, to reduce serum ldl level -c, for the treatment of a cholesterol-related disorder, methods for treating a disorder associated with an abnormal level of ldl-c, a condition associated with a high level of ldl-c, dyslipidemia, hypercholesterolemia, uses of a pcsk9 inhibitor and method for identifying a candidate compound as a pcsk9 inhibitor that binds an epitope of seq id # 1 |
JOP20190150A1 (en) * | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | Pcsk9 antagonist compounds |
-
2020
- 2020-12-18 EP EP20901412.5A patent/EP4076492A4/en active Pending
- 2020-12-18 US US17/757,622 patent/US20230144324A1/en active Pending
- 2020-12-18 WO PCT/US2020/066046 patent/WO2021127460A1/en unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013041678A1 (en) * | 2011-09-23 | 2013-03-28 | Novo Nordisk A/S | Novel glucagon analogues |
Non-Patent Citations (4)
Title |
---|
ALLEYNE CANDICE ET AL: "Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 22, 10 November 2020 (2020-11-10), US, pages 13796 - 13824, XP055881861, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.0c01084 * |
CALLMANN CASSANDRA E. ET AL: "Antitumor Activity of 1,18-Octadecanedioic Acid-Paclitaxel Complexed with Human Serum Albumin", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 141, no. 30, 18 July 2019 (2019-07-18), pages 11765 - 11769, XP055914350, ISSN: 0002-7863, Retrieved from the Internet <URL:http://pubs.acs.org/doi/pdf/10.1021/jacs.9b04272> DOI: 10.1021/jacs.9b04272 * |
See also references of WO2021127460A1 * |
TUCKER THOMAS J. ET AL: "A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 64, no. 22, 27 October 2021 (2021-10-27), US, pages 16770 - 16800, XP093069687, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.1c01599 * |
Also Published As
Publication number | Publication date |
---|---|
EP4076492A1 (en) | 2022-10-26 |
WO2021127460A1 (en) | 2021-06-24 |
US20230144324A1 (en) | 2023-05-11 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
IL279363A (en) | Pcsk9 antagonist compounds | |
EP3956033A4 (en) | Bicyclic compounds | |
EP3836923A4 (en) | Pyrrolo - dipyridine compounds | |
EP3810129A4 (en) | Pcsk9 antagonist bicyclo-compounds | |
EP3843714A4 (en) | Cd73 inhibitors | |
EP3787635A4 (en) | Cd73 inhibitors | |
EP4076492A4 (en) | Pcsk9 antagonist compounds | |
EP4051688A4 (en) | Cd73 inhibitors | |
EP3992176A4 (en) | Ep2 antagonist | |
EP3965792A4 (en) | Hmgb1 antagonist | |
EP4077318A4 (en) | Compounds | |
EP4003986A4 (en) | Inhibitor compounds | |
EP3999517A4 (en) | Cd73 inhibitors | |
EP3950778A4 (en) | Fluoropolyether-group-containing compound | |
EP3956341A4 (en) | Cd73 inhibitors | |
EP3773566A4 (en) | Ox2r compounds | |
EP4034343A4 (en) | Sawhorse | |
EP3998262A4 (en) | Nrf2-activating compound | |
EP3991730A4 (en) | Neurokinin-1 antagonist | |
EP3950780A4 (en) | Fluoropolyether-group-containing compound | |
EP4083032A4 (en) | Pd-l1 antagonist compound | |
EP3929188A4 (en) | Pd-l1 antagonist compound | |
EP3976797A4 (en) | Anti-crispr inhibitors | |
EP4317153A4 (en) | Abhd6 antagonist | |
EP4003201A4 (en) | Bone-binding compounds |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE |
|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE |
|
17P | Request for examination filed |
Effective date: 20220714 |
|
AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR |
|
DAV | Request for validation of the european patent (deleted) | ||
DAX | Request for extension of the european patent (deleted) | ||
P01 | Opt-out of the competence of the unified patent court (upc) registered |
Effective date: 20230529 |
|
A4 | Supplementary search report drawn up and despatched |
Effective date: 20231214 |
|
RIC1 | Information provided on ipc code assigned before grant |
Ipc: A61K 47/54 20170101ALI20231208BHEP Ipc: C12N 9/64 20060101ALI20231208BHEP Ipc: C07K 7/64 20060101ALI20231208BHEP Ipc: C07K 7/06 20060101ALI20231208BHEP Ipc: A61P 3/06 20060101ALI20231208BHEP Ipc: A61K 38/00 20060101AFI20231208BHEP |